GLPG0187-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGLPG0187Cat.No.:HY-100506CASNo.:1320346-97-1分⼦式:C₂₉H₃₇N₇O₅S分⼦量:595.71作⽤靶点:Integrin作⽤通路:Cytoskeleton储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:12.5mg/mL(20.98mM;ultrasonicandwarmingandheatto60°C)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6787mL8.3933mL16.7867mL5mM0.3357mL1.6787mL3.3573mL10mM0.1679mL0.8393mL1.6787mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1.25mg/mL(2.10mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(2.10mM);Clearsolution3.请依序添加每种溶剂：20%HP-β-CDinsalineSolubility:10mg/mL(16.79mM);Suspensionsolution;Needultrasonic4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥0.89mg/mL(1.49mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥0.89mg/mL(1.49mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GLPG0187⼴谱的integrin受体拮抗剂，具有抗肿瘤活性；抑制αvβ1-integrin的IC50值为1.3nM。GLPG0187抑制细胞迁移体⽣物合成⽽⽆细胞毒性。IC50&TargetIC50:1.3nM(αvβ1)[1]体外研究Inasolid-phaseassay,GLPG0187showsselectivityforseveralRGDintegrinreceptorswithIC50sof1.3,3.7,2.0,1.4,1.2,7.7nMforαvβ1,αvβ3,αvβ5,αvβ6,αvβ8,andα5β1.GLPG0187isapotentinhibitorofosteoclasticboneresorptionandangiogenesis.TreatmentwithGLPG0187dose-dependentlyincreasestheE-cadherin/vimentinratio,renderingthecellsamoreepithelial,sessilephenotype.GLPG0187dose-dependentlydiminishesthesizeofthealdehydedehydrogenasehighsubpopulationofprostatecancercells[1].GLPG0187treatmentresultsincellroundingandclumping.GLPG0187demonstratesadose-dependentsignificantreductionintumourcellmigration.GLPG0187atallconcentrationssignificantlyreducescellproliferation[2].体内研究Blockingαv-integrinsbyGLPG0187markedlyreducestheirmetastatictumorgrowth.Bonetumorburdenissignificantlylowerandthenumberofbonemetastases/mouseissignificantlyinhibited.Theprogressionofbonemetastasesandtheformationofnewbonemetastasesduringthetreatmentperiodissignificantlyinhibited[1].PROTOCOLCellAssay[2]TumourcellproliferationisdeterminedusingtheMTSassay.PC3cellsareseededat10,000cells/wellin96wellplatescontainingeitherGLPG0187(0.5,5,or50ng/mL),vehicleormediacontrol,thenculturedin100µLmediumfor24hr.Cellproliferationisanalysedusing20µLMTSdyeincubatedfor3hrat37°Cinthedark.Absorbancefromeachwell(6/treatment)isquantifiedat490nmandthemeanfluorescencecalculated.Theassayisrepeatedat48,72and96hr,onthreeindependentoccasions[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:TheeffectofGLPG0187onbonelossisevaluatedin3-month-oldcastratedmalemiceafter4weeksofAdministration[1]treatmentwithdosingstartingimmediatelyaftercastration(preventiveprotocol).Twodifferentmodesof2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEadministrationareused:eithersubcutaneoustwicedailywith10,30,or100mg/kgofGLPG0187,eitheroral,twicedailywith30,100,or300mg/kgofGLPG0187[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Cell.2021Sep16;184(19):4919-4938.e22.•Gut.2021Jan19;gutjnl-2020-323719.•OxidMedCellLongev.2020May16;2020:6384803.•JPharmaceutBiomed.2021Feb20;195:113825.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PuzhongLu,etal.ChemicalscreeningidentifiesROCK1asaregulatorofmigrasomeformation.CellDiscov.2020Aug4;6(1):51.[2].vanderHorstG,etal.Targetingofα(v)-integrinsinstem/progenitorcellsandsupportivemicroenvironmentimpairsbonemetastasisinhumanprostatecancer.Neoplasia.2011Jun;13(6):516-25.[3].ReevesKJ,etal.Prostatecancercellshometoboneusinganovelinvivomodel:modulationbytheintegrinantagonistGLPG0187.IntJCancer.2015